MM College of Pharmacy, Department of Pharmaceutical Chemistry, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Hr, 133207, India.
Med Chem. 2022;18(8):859-870. doi: 10.2174/1573406418666220214085856.
In the present-day scenario, heterocyclic derivatives have revealed the primary function of various medicinal agents precious for humanity. Out of a diverse range of heterocycles, Styrylquinolines scaffolds have been proved to play an essential role in a broad range of biological activities, including anti-HIV-1, antimicrobial, anti-inflammatory, anti-Alzheimer activity with antiproliferative effects on tumor cell lines. Due to the immense pharmacological importance, distinct synthetic methods have been executed to attain new drug entities from Styrylquinolines. Various schemes for synthesizing Styrylquinolines derivatives like one-pot, ultrasound-promoted heterogeneous acid-catalysed, microwave-assisted, solvent-free, and green synthesis were discussed in the present review. Some products of Styrylquinolines are in clinical trials, and patents are also granted for the novel synthesis of Styrylquinolines. According to the structure-activity relationship, replacement at the R-7 and R-8 positions is required for various activities. In this review, recent synthetic approaches in the medicinal chemistry of Styrylquinolines and potent Styrylquinolines derivatives based on structural activity relationships (SAR) are outlined. Moreover, their primary methods and modifications are also discussed.
在当今的情况下，杂环衍生物已经揭示了对人类具有重要意义的各种药用试剂的主要功能。在众多的杂环中，苯乙烯基喹啉支架已被证明在广泛的生物活性中发挥着重要作用，包括抗 HIV-1、抗菌、抗炎、抗阿尔茨海默病活性以及对肿瘤细胞系的抗增殖作用。由于其巨大的药理学重要性，已经采用了不同的合成方法来从苯乙烯基喹啉中获得新的药物实体。本文综述了各种合成苯乙烯基喹啉衍生物的方法，如一锅法、超声促进多相酸催化、微波辅助、无溶剂和绿色合成等。一些苯乙烯基喹啉的产物正在进行临床试验，并且还为苯乙烯基喹啉的新合成授予了专利。根据构效关系，需要在 R-7 和 R-8 位置进行取代以获得各种活性。在本文综述中，概述了苯乙烯基喹啉的药物化学中的最新合成方法以及基于结构活性关系（SAR）的有效苯乙烯基喹啉衍生物。此外，还讨论了它们的主要方法和修饰。
